1. Field of Invention
GAMMA-Piperidino-butyrophenones; central depressant, neuroleptic compounds.
2. Prior Art
A number of ketones of the general formula ##STR1## wherein R.sub.3 and R.sub.4 are widely different groups, have been made and tested.
Janssen (Cavallito; "Structure-Activity Relationships I", page 37) has stated that one of the groups R.sub.3 and R.sub.4 must be aromatic and that only one may be hydrogen if the ketone is to be an antipsychotic.
For comparison with the compounds of the present invention, we have used two clinically-established piperidino ketones, namely: Haloperidol, wherein ##STR2## AND Methylperon, wherein R.sub.3 .dbd. H and R.sub.4 .dbd. CH.sub.3.
Several compounds having the above-mentioned general formula have also been described in the literature as having, for instance, tranquilizing, central blocking, analgetic, antipyretic, and antiphlogistic properties.
In that context, for instance, compounds are described wherein:
R.sub.3 .dbd. oh or acyloxy and R.sub.4 .dbd. lower alkyl. (See Brit. pat. 1,131,534; Jap. pat. appl. 4,718,877.)
However, the established clinically-useful compounds of the prior art have pronounced shortcomings and side-effects, and there is a clear demand for more specific and advantageous compounds in this activity and utility area, especially as neuroleptics (anti-psychotics). The fulfillment of this demand is one of the objects of the present invention, as further elucidated hereinafter.